Lipopeptid for restraining HIV with broad spectrum, derivatives, drug compound and application thereof

A derivative, HIV-2 technology, applied in the direction of microorganisms, biochemical equipment and methods, peptides, etc., can solve problems such as short biological half-life

Active Publication Date: 2017-05-31
INST OF PATHOGEN BIOLOGY CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, an obvious defect of polypeptide drugs is their short biological half-life, such as the half-life of T-20 is only 3.8 hours, so clinical treatment of patients requires frequent injections of large doses (90mg / time, 2 times / day)

Method used

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  • Lipopeptid for restraining HIV with broad spectrum, derivatives, drug compound and application thereof
  • Lipopeptid for restraining HIV with broad spectrum, derivatives, drug compound and application thereof
  • Lipopeptid for restraining HIV with broad spectrum, derivatives, drug compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0162] Embodiment 1, the design of lipopeptide

[0163] In this example, lipopeptides with the activity of inhibiting HIV-1 and / or HIV-2 and / or SIV are designed, and their names are LP-19, LP-20, LP-21, LP-22, LP-23, LP-24, LP-25, LP-26, LP-27, LP-28, LP-29, LP-30, LP-31 and LP-32, their structures are as figure 1 shown.

Embodiment 2

[0164] Embodiment 2, the preparation of polypeptide and lipopeptide

[0165] 1. Preparation of polypeptides

[0166] The amino-terminals of the polypeptides T-20 and 2P23 are connected with acetyl groups as the amino-terminal protecting group, and the carboxy-terminals are connected with amino groups as the carboxy-terminal protecting group. The structures of these polypeptides are as follows: figure 2 shown. These peptides were synthesized by standard solid-phase peptide synthesis method (Fmoc / tBu strategy), manually synthesized from the carboxy-terminus to the amino-terminus. All polypeptide sequences are amidated at the C-terminus and acetylated at the N-terminus according to the routine of peptide synthesis. Amino acid protected by N-fluorenylmethoxycarbonyl (Fmoc), Rink resin (substitution constant is 0.44mmol / g) is used as a solid phase carrier, and the amino protecting group is removed with a DMF solution of 25% (volume percentage) piperidine For Fmoc, each removal ...

Embodiment 3

[0180] Example 3, detection of broad-spectrum antiviral activity of lipopeptide

[0181] 3.1 Experimental materials and methods

[0182] 3.1.1 Inhibitory effect of lipopeptide on cell fusion mediated by HIV and SIV

[0183] For the materials and methods of the HIV-1, HIV-2 and SIV-mediated cell fusion inhibition experiments, refer to the literature published by Xiong S et al. (Reference 13 in the Background Art). Among them, HEK293T cells (referred to as 239T cells) were purchased from the American Type Culture Collection (ATCC); U87CD4+CXCR4+ cells were provided by the American NIH AIDS Reagent and Reference Project (catalogue number: 4036); HIV-2 strain ROD molecular Cloned plasmid pROD was kindly provided by Prof. Nuno Taveira, University of Lisbon, Portugal; expresses SIV strain SIV pbj and SIV 239 The plasmids of the envelope protein (pSIVpbj-Env and pSIV239 respectively) were donated by Professor Xu Jianqing of Fudan University; the fluorescent reporter system plasmid...

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PUM

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Abstract

The invention discloses a lipopeptid for restraining HIV with a broad spectrum, derivatives, a drug compound and an application thereof. The lipopeptid is a) or b) as follows: a) the lipopeptid comprises a polypeptide, a connecting arm, an amino acid X residual group and a lipotropy compound, wherein the polypeptide has an antiviral activity, the connecting arm is connected with the carboxyl terminal of the polypeptide, the amino acid X residual group is connected with the connecting arm and the lipotropy compound is connected with the amino acid X residual group; b) the lipopeptid comprises the polypeptide and the lipotropy compound, wherein the polypeptide has the antiviral activity and the lipotropy compound is connected with the carboxyl terminal of the polypeptide; the virus is any one of v1 to v7 as follows: v1, HIV-1, HIV-2 and SIV; v2, HIV-1 and HIV-2; v3, HIV-1 and SIV; v4, HIV-2 and SIV; v5 and HIV-1; v6 and HIV-2; v7 and SIV; the amino acid X is K, C, S, T or Y. The lipopeptid can be used for treating and / or preventing HIV infection.

Description

technical field [0001] The invention relates to a lipopeptide for broad-spectrum inhibition of HIV in the field of biomedicine, its derivatives, its pharmaceutical composition and its application. Background technique [0002] There are two types of human immunodeficiency virus (HIV) that cause AIDS (AIDS), type 1 and type 2. At present, the number of HIV infections in the world is about 36 million, HIV-1 is the main pathogen, and about 1-2 million people are caused by HIV-2 infection, mostly in West Africa. However, HIV-2 has gradually spread to Europe, Asia and North America, posing a serious threat to human health [1]. Vaccines are the best way to prevent AIDS, but it is unlikely that there will be a major breakthrough in an effective AIDS vaccine in the near future. Therefore, the research and development of drugs that block the different replication stages of the virus is a key strategy for the prevention and control of AIDS. Since the currently clinically used AIDS ...

Claims

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Application Information

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IPC IPC(8): C07K14/155A61K39/21A61K47/10A61P31/18A61P31/14
CPCA61K39/12A61K47/34C07K14/005C12N2740/15022C12N2740/15034C12N2740/16222C12N2740/16234Y02P20/55
Inventor 何玉先种辉辉丁晓慧熊胜文朱园美
Owner INST OF PATHOGEN BIOLOGY CHINESE ACADEMY OF MEDICAL SCI
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